Systemic exposure without affecting its apparent liver exposures

Molecular Pharmacology

Volumn 83, Issue 5, 2013, Pages 919-929

  Iusuf, Dilek ^a   Van Esch, Anita ^a   Hobbs, Michael ^b   Taylor, Maxine ^b   Kenworthy, Kathryn E ^b   Van De Steeg, Evita ^a   Wagenaar, Els ^a   Schinkel, Alfred H ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CARRIER PROTEIN; ORGANIC ANION TRANSPORTING POLYPEPTIDE 1A; ORGANIC ANION TRANSPORTING POLYPEPTIDE 1B; ROSUVASTATIN; UNCLASSIFIED DRUG; FLUOROBENZENE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; ORGANIC ANION TRANSPORTER; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG EXCRETION; FEMALE; INTESTINE ABSORPTION; KIDNEY; KIDNEY CLEARANCE; LIVER; MOUSE; NONHUMAN; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; SMALL INTESTINE; WILD TYPE; ANIMAL; KNOCKOUT MOUSE; MALE; METABOLISM; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; BIOLOGICAL TRANSPORT; FEMALE; FLUOROBENZENES; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; INTESTINAL ABSORPTION; KIDNEY; LIVER; MALE; MEMBRANE TRANSPORT PROTEINS; MICE; MICE, KNOCKOUT; ORGANIC ANION TRANSPORTERS; PYRIMIDINES; SULFONAMIDES;

EID: 84876520840     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.112.081927     Document Type: Article

References (40)

1. Bardelmeijer HA, Beijnen JH, Brouwer KR, Rosing H, Nooijen WJ, Schellens JH, and van Tellingen O (2000) Increased oral bioavailability of paclitaxel by GF120918 in mice through selective modulation of P-glycoprotein. Clin Cancer Res 6:4416-4421.
2. Bergman E, Lundahl A, Fridblom P, Hedeland M, Bondesson U, Knutson L, and Lennernäs H (2009) Enterohepatic disposition of rosuvastatin in pigs and the impact of concomitant dosing with cyclosporine and gemfibrozil. Drug Metab Dispos 37:2349-2358.
3. Chasman DI, Giulianini F, MacFadyen J, Barratt BJ, Nyberg F, and Ridker PM (2012) Genetic determinants of statin-induced low-density lipoprotein cholesterol reduction: The Justification for the Use of Statins in Prevention: An Intervention Trial Evaluating Rosuvastatin (JUPITER) trial. Circ Cardiovasc Genet 5:257-264.
4. Cheng X, Maher J, Chen C, and Klaassen CD (2005) Tissue distribution and ontogeny of mouse organic anion transporting polypeptides (Oatps). Drug Metab Dispos 33: 1062-1073. (Pubitemid 41002790)
5. Choi JH, Lee MG, Cho JY, Lee JE, Kim KH, and Park K (2008) Influence of OATP1B1 genotype on the pharmacokinetics of rosuvastatin in Koreans. Clin Pharmacol Ther 83:251-257. (Pubitemid 351147710)
6. Choi MK, Shin HJ, Choi YL, Deng JW, Shin JG, and Song IS (2011) Differential effect of genetic variants of Na(1)-taurocholate co-transporting polypeptide (NTCP) and organic anion-transporting polypeptide 1B1 (OATP1B1) on the uptake of HMGCoA reductase inhibitors. Xenobiotica 41:24-34.
7. Degorter MK, Urquhart BL, Gradhand U, Tirona RG, and Kim RB (2012) Disposition of atorvastatin, rosuvastatin, and simvastatin in oatp1b22/2 mice and intraindividual variability in human subjects. J Clin Pharmacol 52: 1689-1697.
8. Gridelli B, Scanlon L, Pellicci R, LaPointe R, DeWolf A, Seltman H, Diven W, Shaw B, Starzl T, and Sanghvi A (1986) Cyclosporine metabolism and pharmacokinetics following intravenous and oral administration in the dog. Transplantation 41: 388-391. (Pubitemid 16117872)
9. Hagenbuch B and Meier PJ (2003) The superfamily of organic anion transporting polypeptides. Biochim Biophys Acta 1609:1-18. (Pubitemid 36044060)
10. Hagenbuch B and Meier PJ (2004) Organic anion transporting polypeptides of the OATP/ SLC21 family: Phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties. Pflugers Arch 447:653-665. (Pubitemid 38241451)
11. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, and Kim RB (2006) Drug and bile acid transporters in rosuvastatin hepatic uptake: Function, expression, and pharmacogenetics. Gastroenterology 130:1793-1806.
12. Hobbs M, Parker C, Birch H, and Kenworthy K (2012) Understanding the interplay of drug transporters involved in the disposition of rosuvastatin in the isolated perfused rat liver using a physiologically-based pharmacokinetic model. Xenobiotica 42:327-338.
13. Hu M, Lui SS, Mak VW, Chu TT, Lee VW, Poon EW, Tsui TK, Ko GT, Baum L, and Tam LS et al. (2010) Pharmacogenetic analysis of lipid responses to rosuvastatin in Chinese patients. Pharmacogenet Genomics 20:634-637.
14. Hua WJ, Hua WX, and Fang HJ (2011) The role of OATP1B1 and BCRP in pharmacokinetics and DDI of novel statins. Cardiovasc Ther 30:e234-e241.
15. Iusuf D, Sparidans R W, van Esch A, Hobbs M, Kenworthy K, van de Steeg E, Wagenaar E, Beijnen JH, and Schinkel AH (2012a) Organic anion-transporting polypeptides 1a/1b control the hepatic uptake of pravastatin in mice. Mol Pharm 9: 2497-2504.
16. Iusuf D, van de Steeg E, and Schinkel AH (2012b) Functions of OATP1A and 1B transporters in vivo: Insights from mouse models. Trends Pharmacol Sci 33: 100-108.
17. Jemnitz K, Veres Z, Tugyi R, and Vereczkey L (2010) Biliary efflux transporters involved in the clearance of rosuvastatin in sandwich culture of primary rat hepatocytes. Toxicol In Vitro 24:605-610.
18. Kalliokoski A and Niemi M (2009) Impact of OATP transporters on pharmacokinetics. Br J Pharmacol 158:693-705.
19. Kitamura S, Maeda K, Wang Y, and Sugiyama Y (2008) Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos 36: 2014-2023.
20. Lee E, Ryan S, Birmingham B, Zalikowski J, March R, Ambrose H, Moore R, Lee C, Chen Y, and Schneck D (2005) Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment. Clin Pharmacol Ther 78:330-341. (Pubitemid 41393668)
21. Martin PD, Warwick MJ, Dane AL, Hill SJ, Giles PB, Phillips PJ, and Lenz E (2003) Metabolism, excretion, and pharmacokinetics of rosuvastatin in healthy adult male volunteers. Clin Ther 25:2822-2835. (Pubitemid 37510592)
22. Nezasa K, Higaki K, Matsumura T, Inazawa K, Hasegawa H, Nakano M, and Koike M (2002a) Liver-specific distribution of rosuvastatin in rats: Comparison with pravastatin and simvastatin. Drug Metab Dispos 30:1158-1163. (Pubitemid 35265820)
23. Nezasa K, Higaki K, Takeuchi M, Nakano M, and Koike M (2003) Uptake of rosuvastatin by isolated rat hepatocytes: Comparison with pravastatin. Xenobiotica 33:379-388. (Pubitemid 36688114)
24. Nezasa K, Takao A, Kimura K, Takaichi M, Inazawa K, and Koike M (2002b) Pharmacokinetics and disposition of rosuvastatin, a new 3-hydroxy-3- methylglutaryl coenzyme A reductase inhibitor, in rat. Xenobiotica 32:715-727. (Pubitemid 34984968)
25. Olsson AG, McTaggart F, and Raza A (2002) Rosuvastatin: A highly effective new HMG-CoA reductase inhibitor. Cardiovasc Drug Rev 20:303-328. (Pubitemid 36105783)
26. Ose A, Kusuhara H, Endo C, Tohyama K, Miyajima M, Kitamura S, and Sugiyama Y (2010) Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. Drug Metab Dispos 38:168-176.
27. Pasanen MK, Fredrikson H, Neuvonen PJ, and Niemi M (2007) Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther 82:726-733. (Pubitemid 350114817)
28. Pasanen MK, Neuvonen PJ, and Niemi M (2008) Global analysis of genetic variation in SLCO1B1. Pharmacogenomics 9:19-33. (Pubitemid 351560529)
29. Peng SX, Rockafellow BA, Skedzielewski TM, Huebert ND, and Hageman W (2009) Improved pharmacokinetic and bioavailability support of drug discovery using serial blood sampling in mice. J Pharm Sci 98:1877-1884.
30. Romaine SP, Bailey KM, Hall AS, and Balmforth AJ (2010) The influence of SLCO1B1 (OATP1B1) gene polymorphisms on response to statin therapy. Pharmacogenomics J 10:1-11.
31. Schneck DW, Birmingham BK, Zalikowski JA, Mitchell PD, Wang Y, Martin PD, Lasseter KC, Brown CD, Windass AS, and Raza A (2004) The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther 75: 455-463. (Pubitemid 38534566)
32. Simonson SG, Raza A, Martin PD, Mitchell PD, Jarcho JA, Brown CD, Windass AS, and Schneck DW (2004) Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine. Clin Pharmacol Ther 76:167-177. (Pubitemid 39013406)
33. Sirtori CR, Mombelli G, Triolo M, and Laaksonen R (2011) Clinical response to statins: Mechanism(s) of variable activity and adverse effects. Ann Med 44: 419-432.
34. van de Steeg E, Stránecký V, Hartmannová H, Nosková L, H-rebí-cek M, Wagenaar E, van Esch A, de Waart DR, Oude Elferink RP, and Kenworthy KE et al. (2012) Complete OATP1B1 and OATP1B3 deficiency causes human Rotor syndrome by interrupting conjugated bilirubin reuptake into the liver. J Clin Invest 122: 519-528.
35. van de Steeg E, Wagenaar E, van der Kruijssen CM, Burggraaff JE, de Waart DR, Elferink RP, Kenworthy KE, and Schinkel AH (2010) Organic anion transporting polypeptide 1a/1b-knockout mice provide insights into hepatic handling of bilirubin, bile acids, and drugs. J Clin Invest 120:2942-2952.
36. van Herwaarden AE, Jonker JW, Wagenaar E, Brinkhuis RF, Schellens JH, Beijnen JH, and Schinkel AH (2003) The breast cancer resistance protein (Bcrp1/Abcg2) restricts exposure to the dietary carcinogen 2-amino-1-methyl-6- phenylimidazo [4,5-b]pyridine. Cancer Res 63:6447-6452. (Pubitemid 37255195)
37. van Waterschoot RA, van Herwaarden AE, Lagas JS, Sparidans RW, Wagenaar E, van der Kruijssen CM, Goldstein JA, Zeldin DC, Beijnen JH, and Schinkel AH (2008) Midazolam metabolism in cytochrome P450 3A knockout mice can be attributed to up-regulated CYP2C enzymes. Mol Pharmacol 73: 1029-1036. (Pubitemid 351397908)
38. Varma MV, Rotter CJ, Chupka J, Whalen KM, Duignan DB, Feng B, Litchfield J, Goosen TC, and El-Kattan AF (2011) pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol Pharm 8:1303-1313.
39. Watanabe T, Kusuhara H, Maeda K, Shitara Y, and Sugiyama Y (2009) Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J Pharmacol Exp Ther 328:652-662.
40. Yang CH, Glover KP, and Han X (2010) Characterization of cellular uptake of perfluorooctanoate via organic anion-transporting polypeptide 1A2, organic anion transporter 4, and urate transporter 1 for their potential roles in mediating human renal reabsorption of perfluorocarboxylates. Toxicol Sci 117: 294-302.